Pregnane X receptor

<StructureSection load='1skx' size='350' side='right' caption='Structure of human pregnane X receptor LBD complex with antibiotic rifampicin (PDB entry 1skx)' scene=>

Pregnane X receptor (PXR) is a Nuclear receptor which senses the presence of toxic substances and regulates the expression of proteins which are involved in detoxificaton. PXR is activated by a large range of steroids, antibiotics, bile acids and many herbal compounds. Thus it is a generalized sensor of hydrophobic toxins. When activated, PXR binds to the retinoid X receptor (RXR) and the formed heterodimer binds to hormone response elements on the DNA. PXR, similar to other nuclear receptors contains a ligand-binding domain (LBD) and DNA-binding domain (DBD).

3D structures of pregnane X receptor

Updated on 05-December-2013

1ilg – hPXR LBD – human
3ctb – hPXR/steroid receptor coactivator
4j5w – hPXR LBD + hRXR LBD

PXR complex with ligand

1ilh, 2qnv – hPXR LBD + ligand
1m13 – hPXR LBD + hyperforin
1skx – hPXR LBD + antibiotic
3r8d – hPXR LBD + anti-HIV drug
1nrl, 2o9i – hPXR LBD + nuclear receptor coactivator peptide + ligand
4j5x – hPXR LBD + hRXR LBD + ligand
3hvl – hPXR/steroid receptor coactivator + ligand

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Joel L. Sussman, Michal Harel, Alexander Berchansky